文章基本信息

标题：The Opioid Receptor Selectivity for Trimebutine in Isolated Tissues Experiments and Receptor Binding Studies
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作者：Hiroshi KANETO ; Masakatsu TAKAHASHI ; Joe WATANABE 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1990
卷号：13
期号：7
页码：448-453
DOI：10.1248/bpb1978.13.448
出版社：The Pharmaceutical Society of Japan
摘要：Differences of affinity ot and selectivity for trimebutine between peripheral and central opioid receptors have been investigated. Trimebutine inhibited electrically induced contraction of guinea-pig ileum (GPI) and mouse vas deferens (MVD) but not of rabbit vas deferens, and the inhibition was antagonized by naloxone and, to lesser extent, by nor-binaltorphimine (nor-BNI). The pA₂ values for morphine and trimebutine with naloxone were higher than the values for these compounds with nor-BNI in both GPI and MVD preparations. GPI preparations incubated with a high concentration of morphine or trimebutine developed tolerance ; however, there was no cross-tolerance between them, suggesting difference in the underlying mechanisms. In mouse and guinea-pig brain homogenate trimebutine was about 1/13 as potent as morphine to displace the [³H]naloxone binding, while it has no appreciable affinity for κ-opioid receptors in [³H]U-69593, a selective κ-receptor agonist. These results suggest that trimebutine, showing its low affinity to opioid receptors, possesses μ-receptor selective properties rather than those of κ-opioid receptor in the peripheral tissues and in the central brain homogenate.
关键词：receptor binding assay